Phosphazide - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Means for the treatment of HIV infection

Included in the formulation

Nikavir®

pills inwards

AZT PHARMA KB, LLC Russia

Nikavir®

pills inwards

AZT PHARMA KB, LLC Russia

АТХ:

J.05.A.X Other antiviral drugs

Pharmacodynamics:Has anti-HIV-activetion. Included in viral DNA, violates the elongation of the DNA chain, stops the growth of the viral DNA molecule, inhibits reverse transcription during retroviral replication. It blocks the key replication process of other retroviruses, has antimicrobial activity against Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Candida albicans.

Pharmacokinetics:Absorption is high (the time of complete absorption is 3 hours), bioavailability is 83.7%. Penetrates through the blood-brain barrier and placenta, the concentration in the cerebrospinal fluid is - 15-64% of the initial dose. The half-life is 2.5 hours. It is metabolized in the liver with the formation of glucuronide, which is excreted by the kidneys.

Indications:HIV infection: the stage of secondary diseases (3A, 3B, 3B according to Pokrovsky classification), the stage of acute infection (2A), the primary clinical manifestations (2B, 2B), a decrease in the number of CD4 T-lymphocytes less than 400-500 / HIV more than 20 thousand copies per 1 ml (when determined by RT PCR method), stage of incubation (Article 1); prevention at the risk of HIV infectionI contaminated biological material with pricks, cuts, contact with mucous membranes in laboratories, with surgical, gynecological, dentaloperations and manipulations, during sexual intercourse and intravenous drug use.

ICD-10

I.B20-B24 Disease caused by the human immunodeficiency virus [HIV]

Contraindications:Severe nausea, vomiting, anemia (hemoglobin content below 50 g / l), increased transaminase activity (more than 5 times the upper limit of the norm), hypercreatininemianeutropenia (less than 0.5 ·10⁹/ l ), thrombocytopenia (less than 25 · 10⁹/ l ), pregnancy (the first 14 weeks), breast-feeding.

Carefully:Inhibition of bone marrow hematopoiesis, deficiency of cyanocobalamin or folic acid, hepatic insufficiency, excessive body weight, long-term administration of nucleoside analogues.

Pregnancy and lactation:

Recommendations for FDA - Category C. Qualitative and well-controlled studies on humans and animals have not been conducted. Do not apply!

Penetrates into breast milk. Do not apply!

Dosing and Administration:

Accepted inwards, before eating. The daily dose is taken in 2 divided doses.

Adults - 0.6-1.2 g per day; children - 10-20 mg / kg per day.

With lesions of the central nervous system, the daily dose is 1.2 g; with the development of side effects - 0.4 g per day.

Assign for a long unlimited period; if necessary intermittent courses for at least 3 months.

According to the continuous scheme, treatment is performed in patients with acute HIV infection (Article 2A) for the period of clinical manifestations (plus 1 month after, but not less than 3 months); in Art. 3B - constantly, in art. 3A and 3B - with atypical manifestations. In Art. 3A and 3B (in the phase of absence of clinical manifestations), 2B and 2B are prescribed with CD4 T-lymphocytes from 200 / μL to 500 / μL for 3 months, with a 3-month interval.

For the prevention of HIV infection take no later than 72 hours after the alleged infection of 0.6 g 2 times a day, for 4 weeks.

Side effects:

Anemia, leukopenia, neutropenia, thrombocytosis, less thrombocytopenia.
Hepatotoxicity, pancreatitis, lactic acidosis.
Myopathy, neuropathy.
Anorexia, asthenia, constipation, severe headache, insomnia, weakness, myalgia, nausea, vomiting.
Skin pigmentation, hyperpigmentation of nails.
Abdominal pain, chills, dyspepsia, diarrhea, decreased appetite, flatulence; unusual fatigue or weakness, hyperbilirubinemia, muscle pain, neuralgia.
Oppression of bone marrow hemopoiesis (fever, chills, sore throat, pallor, unusual fatigue or weakness).
Paresthesia, drowsiness,perversion of taste, pain in the heart; increased activity of transaminases and amylases, hypercreatininaemia; development of secondary infection; depression, frequent urination, cough.

Overdose:

Symptoms: vomiting, severe nausea.

Treatment: discontinuation of reception prior to consultation with a physician.

Interaction:

Amphotericin B. The combined use of phosphazide with amphotericin B may result in a mutual enhancement of myelotoxicity, and therefore additional control over the concentration of hemoglobin and the amount of granulocytes is required.

Vinblastine. The combined use of phosphazide with vinblastine may result in a mutual enhancement of myelotoxicity, therefore additional control over the concentration of hemoglobin and the amount of granulocytes is required.

Vincristine. The combined use of phosphazide with vincristine can result in a mutual enhancement of myelotoxicity, therefore additional control is required for the concentration of hemoglobin and the amount of granulocytes.

Ganciclovir. The combined use of phosphazide with ganciclovir can lead to mutual enhancement of myelotoxicity, therefore additional control over the concentration of hemoglobin and the amount of granulocytes is required.

Dapson. The combined use of phosphazide with dapsone may result in a mutual enhancement of myelotoxicity, so additional monitoring of the concentration of hemoglobin and the amount of granulocytes is required.

Didanosine. The combined use of phosphazide with didanosine leads to a mutual increase in activity against HIV.

Doxorubicin. The combined use of phosphazide with doxorubicin can result in a mutual enhancement of myelotoxicity, therefore additional control is required for the concentration of hemoglobin and the amount of granulocytes.

Zidovudine. The combined use of phosphazide with zidovudine results in a mutual decrease in activity against HIV.

Interferon-alpha. The combined use of phosphazide with interferon-alpha leads to a mutual increase in activity against HIV. The combined use of phosphazide with interferon-alpha can lead to mutual enhancement of myelotoxicity, therefore additional control over the concentration of hemoglobin and the amount of granulocytes is required.

Co-trimoxazole [Sulfamethoxazole + Trimethoprim]. The combined use of phosphazide with co-trimoxazole may result in a mutual enhancement of myelotoxicity,therefore, additional control over the concentration of hemoglobin and the amount of granulocytes is required.

Lamivudine. The combined use of phosphazide with lamivudine results in a mutual increase in activity against HIV.

Stavudine. The combined use of phosphazide with stavudine leads to a mutual decrease in activity against HIV.

Sulfadiazine. The combined use of phosphazide with sulfadiazine may result in a mutual enhancement of myelotoxicity, and therefore additional control over the concentration of hemoglobin and the amount of granulocytes is required.

Special instructions:Used in combination with other antiretroviral drugs in combined treatment regimens, except for the combination with zidovudine and didanosine. Irregular reception (violation of the treatment regimen) can lead to the development of resistance, a decrease in the effectiveness of therapy and the need to replace the drug. With pronounced side effects, the treatment is suspended until the normal state is restored. In assessing the tolerability of the drug should be borne in mind that skin rash, itching, headache nausea and other unwanted phenomena can be a manifestation of the HIV infection itself,concomitant diseases and therapy.

Instructions

Phosphazide (Phosphazidum)